Background: Treatment of metastatic renal cell carcinoma (mRCC) typically entails mechanistically distinct agents across the first- and second-line setting.
Prediction of Losartan Active Carboxylic Acid Metabolite Exposure Following Losartan Administration Using Static and Physiologically-Based Pharmacokinetic Models.
The aim of this study was to evaluate a strategy based on static and dynamic physiologically based pharmacokinetic (PBPK) modeling for the prediction of metabolite and parent drug area under...
Development and qualification of physiologically based pharmacokinetic models for drugs with atypical distribution behavior: A desipramine case study.
Desipramine is a secondary tricyclic amine, which is primarily metabolized by cytochrome 2D6. It shows a high volume of distribution (Vss) (10–50 L/kg) due to its high lipophilicity, unspecific phospholipid binding, and lysosomal trapping.
Food effect: The combined effect of media pH and viscosity on the gastrointestinal absorption of ciprofloxacin tablet
The clinical implications of food-drug interactions may have to be taken seriously into account with oral drugs administration in order to minimize variations in drug bioavailability.
Influence of different proton pump inhibitors on the pharmacokinetics of voriconazole
This study aimed to determine the influence of proton pump inhibitors (PPIs) on the pharmacokinetics of voriconazole and to characterise potential drug-drug interactions (DDIs)...
Systems pharmacology modeling of drug-induced hyperbilirubinemia: Differentiating hepatotoxicity and inhibition of enzymes/transporters
Elevations in serum bilirubin during drug treatment may indicate global liver dysfunction and a high risk of liver failure.
In vitro dissolution models for the prediction of in vivo performance of an oral mesoporous silica formulation
Drug release from mesoporous silica systems has been widely investigated in vitro using USP Type II (paddle) dissolution apparatus.
Mechanistic prediction of food effects for Compound A tablet using PBPK model
Physiologically based pharmacokinetic (PBPK) modeling has been extensively used to study the factors of effect drug absorption, distribution, metabolize and extraction progress in human.
Biopharmaceutics data management system for anonymised data sharing and curation: First application with orbito IMI project
The OrBiTo IMI project was designed to improve the understanding and modelling of how drugs are absorbed.
In silico-in vitro-in vivo studies of experimentally designed carvedilol loaded silk fibroin-casein nanoparticles using physiological based pharmacokinetic model
The study aimed to design and develop carvedilol loaded silk fibroin-casein nanoparticles using 32 full factorial design.
Design and evaluation of an extended-release matrix tablet formulation; the combination of hypromellose acetate succinate and hydroxypropylcellulose
The purpose of this study was to develop an extended-release (ER) matrix tablet that shows robust dissolution properties able to account for the variability of pH and mechanical stress in the GI tract using...
Synthesis, spectral characterization, crystal structure, cytotoxicity and apoptosis—Inducing activity of two derivatives of 2-hydroxy-1,4-naphthaquinone
A phenaxazone compound [5H-Benzo[a]phenoxazin-5-one (BP)] along with an aminoquinone[2-[(o-hydroxyphenyl)amino]-1,4-naphthaquinone (HAN)] derivatives were synthesized from...
Characterising Drug Release from Immediate-Release Formulations of a Poorly Soluble Compound, Basmisanil, Through Absorption Modelling and Dissolution Testing
The study aimed to characterise the mechanism of release and absorption of Basmisanil, a biopharmaceutics classification system (BCS) class 2 compound, from immediate-release formulations via mechanistic absorption modelling, dissolution testing, and Raman imaging.
Discovery of N-(pyridin-4-yl)-1,5-naphthyridin-2-amines as potential tau pathology PET tracers for Alzheimer’s Disease.
A mini-HTS on 4000 compounds selected using 2D fragment-based similarity and 3D pharmacophoric and shape similarity to known selective tau aggregate binders identified N-(6-methylpyridin-2-yl)...
Intracellular drug bioavailability: a new predictor of system dependent drug disposition
Intracellular drug exposure is influenced by cell- and tissue-dependent expression of drug-transporting proteins and metabolizing enzymes.
Mechanistic understanding of the effect of renal impairment on metformin oral absorption using computer simulations
The physiological parameters that describe the reasons behind metformin accumulation in renal failure patients are not fully understood.
Vitamin K epoxide reductase regulation of androgen receptor activity
Long-term use of warfarin has been shown to be associated with a reduced risk of prostate cancer. Warfarin belongs to the vitamin K antagonist class of anticoagulants, which...
Identification, characterization and in silico ADMET prediction of Roflumilast degradation products
The present study reports the degradation behavior of roflumilast (RFL), a new drug developed for the treatment of chronic obstructive pulmonary disease.
Progress in Prediction and Interpretation of Clinically Relevant Metabolic Drug-Drug Interactions: a Minireview Illustrating Recent Developments and Current Opportunities
This review gives a perspective on the current “state of the art” in metabolic drug-drug interaction (DDI) prediction.